Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives.

Saku O; Saki M; Kurokawa

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Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives.

机译：选择性腺苷A2A受体拮抗剂的合成研究：新型苯并呋喃衍生物的合成与构效关系。

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A series of benzofuran derivatives were prepared to study their antagonistic activities to the A(2A) receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modifications of the amide moiety showed enhanced antagonistic activity. From these studies, compounds 13c, 13f, and 24a showed good potency in vitro and were identified as novel A(2A) receptor antagonists suitable for oral activity evaluation in animal models of catalepsy.

机译：制备了一系列的苯并呋喃衍生物以研究其对A（2A）受体的拮抗活性。用苯环取代先导化合物1的酯基改善了PK分布，而酰胺部分的修饰显示出增强的拮抗活性。从这些研究中，化合物13c，13f和24a在体外显示出良好的效能，并被确定为适用于僵尸动物模型中口服活性评估的新型A（2A）受体拮抗剂。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共4页
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Saku O; Saki M; Kurokawa;
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1. Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives. [J] . Saku O, Saki M, Kurokawa Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：选择性腺苷A2A受体拮抗剂的合成研究：新型苯并呋喃衍生物的合成与构效关系。
2. Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives. [J] . Saku O, Saki M, Kurokawa Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：选择性腺苷A2A受体拮抗剂的合成研究：新型苯并呋喃衍生物的合成与构效关系。
3. Synthetic studies on selective adenosine A2A receptor antagonists. Part II: synthesis and structure-activity relationships of novel benzofuran derivatives. [J] . Saku O, Saki M, Kurokawa M, Bioorganic and Medicinal Chemistry Letters . 2010,第12期

机译：选择性腺苷A2A受体拮抗剂的合成研究。第二部分：新型苯并呋喃衍生物的合成及其构效关系。
4. 3D-Pharmacophore Models for Selective A2A and A2B Adenosine Receptor Antagonists [C] . Jing Wei, Songqing Wang, Shaofen Gao, 第三届国际分子模拟与信息技术应用学术会议 . 2007

机译：选择性A2A和A2B腺苷受体拮抗剂的3D药理模型
5. Selective GLP-1 receptor antagonists and glucagon/GLP-1 co-agonists discovered through an investigation into the structure-activity relationship in glucagon-related peptides. [D] . Patterson, James T. 2011

机译：通过研究胰高血糖素相关肽的结构-活性关系，发现了选择性的GLP-1受体拮抗剂和胰高血糖素/ GLP-1共激动剂。
6. Structure-Activity Relationships of Truncated Adenosine Derivatives as Highly Potent and Selective Human A3 Adenosine Receptor Antagonists [O] . Shantanu Pal, Won Jun Choi, Seung Ah Choe, -1

机译：截断腺苷衍生物作为高效性和选择性人A3腺苷受体拮抗剂的结构 - 活性关系
7. Development of Dual-Acting Benzofurans for Thromboxane A2 Receptor Antagonist and Prostacyclin Receptor Agonist: Synthesis, Structure-Activity Relationship, and Evaluation of Benzofuran Derivatives [O] . -1

机译：血栓素A2受体拮抗剂和前列环素受体激动剂的双作用苯呋喃的发展：合成，结构 - 活性关系和苯并呋喃衍生物的评价

Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives.

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